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BMS-777607

Cat. No. M1682
BMS-777607 Structure
Synonym:

CAS# 1025720-94-8

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 72  USD72 In stock
10mg USD 120  USD120 In stock
50mg USD 360  USD360 In stock
100mg USD 620  USD620 In stock
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Quality Control
Biological Activity

BMS-777607 is a selective and potent small-molecule met kinase inhibitor. Overexpression of c-Met receptor tyrosine kinase has been highly associated with prostate cancer progression and metastasis. BMS-777607 suppressed HGF-stimulated cell migration and invasion in a dose-dependent fashion (IC50 < 0.1 μmol/L). Mechanistically, nanomolar doses of BMS 777607 potently blocked HGF-stimulated c-Met autophosphorylation and downstream activation of Akt and extracellular signal-regulated kinase.

Customer Product Validations & Biological Datas
Source Mol Oncol (2014). Figure 2. BMS-777607
Method Western blot
Cell Lines breast cancer cells
Concentrations 5 μM
Incubation Time 72 h
Results Thus, results demonstrate that expression of p21/WAF1 and survivin is up-regulated in BMS-777607 induced polyploid/senescent cells regardless the status of p53.
Source Mol Oncol (2014). Figure 1. BMS-777607
Method senescence detection assay
Cell Lines BMS-777607. T-47D and ZR-75-1 cells
Concentrations 5 μM
Incubation Time 72 h
Results The percentages of SABG-positive cells were associated with increased doses of BMS-777607.
Protocol
Cell Experiment
Cell lines PC-3 cell line
Preparation method Cell proliferation and cell death Cells were seeded in a 96-well plate at a density of 5 × 103 cells per well and exposed to serial dilutions of BMS-777607 for 1 hour. HGF (25 ng/mL) was then added and the cells were incubated (drug plus HGF) for a period of 96 hours. At the end of the treatment period, the tumor cells were exposed to WST-8 (MTT assay reagent) in a Cell Counting kit (Donjindo Molecular Technologies) according to the manufacturer's instruction, and absorbance was determined at 450 nm colorimetrically. Cell proliferation (%) was calculated as the ratio of absorbance from treated sample to the nontreated control. Cell death was examined by trypan blue exclusion, and positively stained (dead) cells were scored using a hemocytometer.
Concentrations 0, 0.1, 0.3, 1, 3, 10 μM
Incubation time 96 h
Animal Experiment
Animal models C3H/HeJ mice with KHT lung tumor model
Formulation DMSO
Dosages 25mg/kg daily
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 512.89
Formula C25H19ClF2N4O4
CAS Number 1196681-44-3
Purity 99.50%
Solubility DMSO 40 mg/mL
Storage at -20°C
References

[1] Dai et al. BMC Cancer. Constitutively active c-Met kinase in PC-3 cells is autocrine-independent and can be blocked by the Met kinase inhibitor BMS-777607.

[2] Dai et al. Clin Exp Metastasis. Impact of the small molecule Met inhibitor BMS-777607 on the metastatic process in a rodent tumor model with constitutive c-Met activation.

[3] Dai et al. Mol Cancer Ther. BMS-777607, a small-molecule met kinase inhibitor, suppresses hepatocyte growth factor-stimulated prostate cancer metastatic phenotype in vitro.

[4] Schroeder et al. J Med Chem. Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a selective and orally efficacious inhibitor of the Met kinase superfamily.

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Keywords: BMS-777607, CAS# 1025720-94-8 supplier, c-Met, inhibitors

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